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Correlating gastric emptying of amphotericin B and paracetamol solid lipid nanoparticles with changes in particle surface chemistry

Amekyeh, Hilda; Billa, Nashiru; Roberts, Clive J.

Correlating gastric emptying of amphotericin B and paracetamol solid lipid nanoparticles with changes in particle surface chemistry Thumbnail


Authors

Hilda Amekyeh

Nashiru Billa



Abstract

Oral delivery of pharmaceuticals requires that they retain their physical and chemical attributes during transit within the gastrointestinal (GI) tract, for the manifestation of desired therapeutic profiles. Solid lipid nanoparticles (SLNs) are used as carriers to improve the absorption of hydrophobic drugs. In this study, we examine the stability of amphotericin B (AmB) and paracetamol (PAR) SLNs in simulated GI fluids during gastric emptying. On contact with the simulated fluids, the particles increased in size due to ingress of the dissolution media into the particles. Simulated gastric emptying revealed that the formulations had mean sizes <350 nm and neutral surface charges, both of which are optimal for intestinal absorption of SLNs. There was ingress of the fluids into the SLNs, followed by diffusion of the dissolved drug, whose rate depended on the solubility of the loaded-drug in the particular medium. Time-of-flight secondary ion mass spectrometry analyses indicated that drug loading followed the core-shell model and that the AmB SLNs have a more drug-enriched core than the PAR SLNs do. The AmB SLNs are therefore a very suitable carrier of AmB for oral delivery. The stability of the SLNs in the simulated GI media indicates their suitability for oral delivery.

Citation

Amekyeh, H., Billa, N., & Roberts, C. J. (2017). Correlating gastric emptying of amphotericin B and paracetamol solid lipid nanoparticles with changes in particle surface chemistry. International Journal of Pharmaceutics, 517(1-2), https://doi.org/10.1016/j.ijpharm.2016.12.001

Journal Article Type Article
Acceptance Date Dec 1, 2016
Online Publication Date Dec 5, 2016
Publication Date Jan 30, 2017
Deposit Date May 23, 2017
Publicly Available Date May 23, 2017
Journal International Journal of Pharmaceutics
Print ISSN 0378-5173
Electronic ISSN 1873-3476
Publisher Elsevier
Peer Reviewed Peer Reviewed
Volume 517
Issue 1-2
DOI https://doi.org/10.1016/j.ijpharm.2016.12.001
Keywords Solid lipid nanoparticle; Stability; Gastrointestinal tract; Gastric emptying; Amphotericin B; Paracetamol
Public URL https://nottingham-repository.worktribe.com/output/838552
Publisher URL http://www.sciencedirect.com/science/article/pii/S0378517316311322
Contract Date May 23, 2017

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